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Exploring the synthesis, structure and bioactivity of pyrimidine carboxylic acid-derived organic antimony (V) complexes: Cytostatic and antimicrobial evaluations
Journal of Organometallic Chemistry ( IF 2.3 ) Pub Date : 2024-04-04 , DOI: 10.1016/j.jorganchem.2024.123128
Xin Yao , Jun-Wei Ma , Nian-Tao Yao , Fei Yin , Ru-Fen Zhang

Eight new organoantimony complexes, RSb (R = Ph, -MePh; = L1, L2) and (RSb)O (R = pHPh, -MePh; = L1, L2), [PhSb(CHNO)] (), [(PhSb)O(CHNO)] (), [(-tol)Sb(CHNO)] (), [(-tol)SbO(CHNO)] (), [PhSb(CHNO)] (), [(PhSb)O(CHNO)] (), [(-tol)Sb(CHNO)] () and [(-tol)SbO(CHNO)] (), were designed and synthesized by the reaction of 4-pyrimidine carboxylic acid (HL1) or 5-pyrimidine carboxylic acid (HL2) with organoantimony precursors. All the complexes were characterized by elemental analysis, FT-IR, NMR (H and C), and single crystal X-ray diffraction analysis. Crystal structure results reveal that the central antimony atom of all the complexes displays a triangular biconical geometry. Among them, complexes and show a monomeric structure, while complexes and have a dimeric structure with oxygen bridges. The cytostatic activities of the eight complexes against a human alveolar basal epithelial lung cancer cell lines (A549) and hepatocellular carcinoma cell lines (HepG-2) were investigated, and the results showed that the organoantimony derivatives with the tolyl groups () exhibited higher cytostatic activities compared with those with the phenyl groups (). At the same time, bacteriostatic tests were conducted to assess the inhibitory effects of complexes against three prevalent plant pathogenic fungi and one bacterium. The results revealed that complex exhibited significant fungicidal activities, on the other hand, complex exhibited higher antibacterial activity against MRSA. These results will provide significant guidance for the further exploration of potential efficient biological activity complexes.

中文翻译:

探索嘧啶羧酸衍生的有机锑 (V) 配合物的合成、结构和生物活性:细胞抑制和抗菌评估

八种新的有机锑配合物,RSb (R = Ph, -MePh; = L1, L2) 和 (RSb)O (R = pHPh, -MePh; = L1, L2), [PhSb(CHNO)] (), [(PhSb) )O(CHNO)] (), [(-tol)Sb(CHNO)] (), [(-tol)SbO(CHNO)] (), [PhSb(CHNO)] (), [(PhSb)O(通过4-嘧啶羧酸(HL1)或5的反应设计合成了[(-tol)Sb(CHNO)]()和[(-tol)SbO(CHNO)]()。 -嘧啶羧酸(HL2)与有机锑前体。所有配合物均通过元素分析、FT-IR、NMR(1H 和 C)和单晶 X 射线衍射分析进行了表征。晶体结构结果表明,所有配合物的中心锑原子均呈现三角形双锥几何形状。其中,配合物 和 呈现单体结构,而配合物 和 则具有带氧桥的二聚结构。研究了八种配合物对人肺泡基底上皮肺癌细胞系(A549)和肝细胞癌细胞系(HepG-2)的细胞抑制活性,结果表明,带有甲苯基()的有机锑衍生物表现出更高的细胞抑制活性。与带有苯基的活性相比()。同时,进行抑菌试验,评估复合物对三种常见植物病原真菌和一种细菌的抑制效果。结果表明,复合物表现出显着的杀菌活性,同时,复合物对MRSA也表现出较高的抗菌活性。这些结果将为进一步探索潜在的高效生物活性复合物提供重要指导。
更新日期:2024-04-04
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